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Picamilon is able to cross the blood–brain barrier[5] and then is hydrolyzed into GABA and niacin. The released GABA in theory would activate GABA receptors potentially producing an anxiolytic response.[6] The second released component, niacin acts as a strong vasodilator,[7] which might be useful for the treatment of migraine headaches.[8][9]

...Taken on its own, Niacin is a water-soluble B vitamin that easily crosses the blood-brain barrier. It functions to protect neurons against the effects of diminished blood flow...Because this drug can easily penetrate the blood-brain barrier,improve brain blood flow ...

...Studies show that Picamilon dramatically increases blood flow and circulation within the brain...Picamilon increases blood supply and functional state of the brain, increases microcirculation and hemodynamics of the eyes... and vasoactive agent for acute ischemic disturbances of the cerebral blood circulation of mild to moderate severity...In opthalmological practice, for primary open-angle glaucoma with normalized intraocular pressure, and for diseases of the retina and the optic nerve....